Affinity (pKd or pKi) of CXCR2 ligands at site-directed mutagenesis CXCR2 human or baboon mutants to probe human-baboon species differences
Displacement of 125I-CXCL8 binding to COS-7 cell membranes expressing indicated human-to-baboon or baboon-to-human CXCR2 mutants. The data are presented as mean ± S.E.M. of at least three independent experiments.
| CXCR2 | pKd CXCL8 | pKi | |
|---|---|---|---|
| SB265610 | Compound 1 | ||
| Human | |||
| WT | 9.40 ± 0.14 | 7.68 ± 0.11 | 7.18 ± 0.13 |
| S2175.44T | 9.20 ± 0.11 | 7.92 ± 0.06 | 5.77 ± 0.12 |
| N2686.52H | 9.18 ± 0.11 | 7.14 ± 0.08 | <5 |
| S2175.44T/N2686.52H | 9.43 ± 0.20 | 7.27 ± 0.16 | <4 |
| Q2806.64R | 9.13 ± 0.04 | 7.29 ± 0.14 | 7.10 ± 0.11 |
| V2816.65L | 9.17 ± 0.16 | 7.33 ± 0.14 | 7.22 ± 0.09 |
| Q2836.67N | 9.41 ± 0.09 | 7.24 ± 0.16 | 7.07 ± 0.17 |
| E2876.71Q | 9.11 ± 0.11 | 7.39 ± 0.25 | 6.99 ± 0.12 |
| R2947.33Q | 9.15 ± 0.12 | 7.24 ± 0.16 | 7.04 ± 0.12 |
| Baboon | 9.33 ± 0.08 | 7.28 ± 0.10 | <4 |
| T2125.44S | 9.89 ± 0.29 | 7.10 ± 0.13 | <5 |
| H2636.52N | 9.69 ± 0.19 | 6.85 ± 0.21 | 5.72 ± 0.13 |
| T2125.44S/H2636.52N | 9.61 ± 0.08 | 7.13 ± 0.17 | 7.40 ± 0.14 |